Subramanian G, McAfee J G, Blair R J, Kallfelz F A, Thomas F D
J Nucl Med. 1975 Aug;16(8):744-55.
Methylene diphosphonate (MDP) was formulated as a complex of 99mTc for skeletal imaging. This agent was compared with three other bone-seeking technetium agents: ethane-1-hydroxy-1, 1-diphosphonate (EHDP), pyrophosphate, and polyphosphate. In tissue radioassay experiments in rodents, the technetium complexes of MDP and EHDP were similar, but skeletal concentration with both of these agents was higher than that with pyrophosphate or polyphosphate. The total-body retention of MDP and EHDP complexed with 95mTc was studied in beagle dogs for 35 days by excretion measurements and total-body counting and compared with polyphosphate and pertechnetate. The long-term retention was greater for MDP. The 5-day cumulative fecal excretion of 95mTc was low when administered as EHDP or polyphosphate complexes and negligible when administered as MDP complex. In six human volunteers the blood clearance of 99mTc-mdp was similar to that of 18F and significantly faster than that of 99mTc-EHDP. Pyrophosphate cleared from the blood much faster than polyphosphate but slower than the diphosphonates. The urinary excretion of the MDP complex was greater than for EHDP within the first 2-3 hr after injection. The 24-hr urinary excretion of pyrophosphate and polyphosphate complexes was not as complete as for the diphosphonates. All four 99mTc complexes proved satisfactory for clinical imaging studies. The MDP complex produced images of superior quality as early as 2 hr after administration, attributable to its more rapid clearance from the blood and soft tissues. On the contrary, a longer interval of 3-4 hr after injection was usually needed for 99mTc-EHDP; pyrophosphate and polyphosphate complexes regularly required a waiting period of 4 hr. Comparitive radiation dose estimates were made based on the available biologic distribution data for these 99mTc skeletal-localizing agents.
亚甲基二膦酸盐(MDP)被制成99mTc的复合物用于骨骼显像。该制剂与其他三种亲骨性锝制剂进行了比较:乙烷-1-羟基-1,1-二膦酸盐(EHDP)、焦磷酸盐和多磷酸盐。在啮齿动物的组织放射性测定实验中,MDP和EHDP的锝复合物相似,但这两种制剂在骨骼中的浓度均高于焦磷酸盐或多磷酸盐。通过排泄测量和全身计数,在比格犬中对与95mTc络合的MDP和EHDP的全身滞留情况进行了35天的研究,并与多磷酸盐和高锝酸盐进行了比较。MDP的长期滞留情况更显著。以EHDP或多磷酸盐复合物形式给药时,95mTc的5天累积粪便排泄量较低,而以MDP复合物形式给药时可忽略不计。在6名人类志愿者中,99mTc-MDP的血液清除率与18F相似,且明显快于99mTc-EHDP。焦磷酸盐从血液中的清除速度比多磷酸盐快得多,但比二膦酸盐慢。注射后最初2 - 3小时内,MDP复合物的尿排泄量大于EHDP。焦磷酸盐和多磷酸盐复合物的24小时尿排泄不如二膦酸盐完全。所有四种99mTc复合物在临床显像研究中均被证明是令人满意的。MDP复合物在给药后2小时就产生了质量上乘的图像,这归因于其从血液和软组织中清除得更快。相反,99mTc-EHDP通常需要注射后3 - 4小时的更长间隔时间;焦磷酸盐和多磷酸盐复合物通常需要等待4小时。基于这些99mTc骨骼定位剂的现有生物分布数据进行了比较辐射剂量估计。